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WO2008021389A3 - Using pi3k and mek modulators in treatments of cancer - Google Patents

Using pi3k and mek modulators in treatments of cancer Download PDF

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Publication number
WO2008021389A3
WO2008021389A3 PCT/US2007/018057 US2007018057W WO2008021389A3 WO 2008021389 A3 WO2008021389 A3 WO 2008021389A3 US 2007018057 W US2007018057 W US 2007018057W WO 2008021389 A3 WO2008021389 A3 WO 2008021389A3
Authority
WO
WIPO (PCT)
Prior art keywords
pi3k
cancer
treatments
mek
modulators
Prior art date
Application number
PCT/US2007/018057
Other languages
French (fr)
Other versions
WO2008021389A8 (en
WO2008021389A2 (en
Inventor
Dana T Aftab
Douglas A Laird
Peter Lamb
Jean-Francois A Martini
Original Assignee
Exelixis Inc
Dana T Aftab
Douglas A Laird
Peter Lamb
Jean-Francois A Martini
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to EP07811344A priority Critical patent/EP2056829B9/en
Priority to CA002658725A priority patent/CA2658725A1/en
Priority to JP2009524671A priority patent/JP2010500994A/en
Priority to US12/373,257 priority patent/US20100075947A1/en
Priority to AT07811344T priority patent/ATE539752T1/en
Priority to AU2007284562A priority patent/AU2007284562B2/en
Application filed by Exelixis Inc, Dana T Aftab, Douglas A Laird, Peter Lamb, Jean-Francois A Martini filed Critical Exelixis Inc
Publication of WO2008021389A2 publication Critical patent/WO2008021389A2/en
Publication of WO2008021389A3 publication Critical patent/WO2008021389A3/en
Publication of WO2008021389A8 publication Critical patent/WO2008021389A8/en
Priority to HK09110424.6A priority patent/HK1130438A1/en
Priority to US13/568,649 priority patent/US8642584B2/en
Priority to US14/099,939 priority patent/US20140100215A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/44—Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.
PCT/US2007/018057 2006-08-16 2007-08-16 Using pi3k and mek modulators in treatments of cancer WO2008021389A2 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
CA002658725A CA2658725A1 (en) 2006-08-16 2007-08-16 Using pi3k and mek modulators in treatments of cancer
JP2009524671A JP2010500994A (en) 2006-08-16 2007-08-16 Methods of using PI3K and MEK modulators
US12/373,257 US20100075947A1 (en) 2006-08-16 2007-08-16 Methods of Using PI3K and MEK Modulators
AT07811344T ATE539752T1 (en) 2006-08-16 2007-08-16 USE OF PI3K AND MEK MODULATORS IN CANCER TREATMENT
AU2007284562A AU2007284562B2 (en) 2006-08-16 2007-08-16 Using PI3K and MEK modulators in treatments of cancer
EP07811344A EP2056829B9 (en) 2006-08-16 2007-08-16 Using pi3k and mek modulators in treatments of cancer
HK09110424.6A HK1130438A1 (en) 2006-08-16 2009-11-09 Using pi3k and mek modulators in treatments of cancer
US13/568,649 US8642584B2 (en) 2006-08-16 2012-08-07 Method of using PI3K and MEK modulators
US14/099,939 US20140100215A1 (en) 2006-08-16 2013-12-07 Methods of Using PI3K and MEK Modulators

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US83830706P 2006-08-16 2006-08-16
US60/838,307 2006-08-16

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US12/373,257 A-371-Of-International US20100075947A1 (en) 2006-08-16 2007-08-16 Methods of Using PI3K and MEK Modulators
US13/568,649 Continuation US8642584B2 (en) 2006-08-16 2012-08-07 Method of using PI3K and MEK modulators

Publications (3)

Publication Number Publication Date
WO2008021389A2 WO2008021389A2 (en) 2008-02-21
WO2008021389A3 true WO2008021389A3 (en) 2008-07-17
WO2008021389A8 WO2008021389A8 (en) 2009-03-12

Family

ID=38819883

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2007/018057 WO2008021389A2 (en) 2006-08-16 2007-08-16 Using pi3k and mek modulators in treatments of cancer

Country Status (9)

Country Link
US (3) US20100075947A1 (en)
EP (1) EP2056829B9 (en)
JP (5) JP2010500994A (en)
CN (2) CN101528231A (en)
AT (1) ATE539752T1 (en)
AU (1) AU2007284562B2 (en)
CA (1) CA2658725A1 (en)
HK (1) HK1130438A1 (en)
WO (1) WO2008021389A2 (en)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9533954B2 (en) 2010-12-22 2017-01-03 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
US9533984B2 (en) 2013-04-19 2017-01-03 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors

Families Citing this family (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2364974A1 (en) * 2005-10-07 2011-09-14 Exelixis, Inc. N-(3-Phenylamino-quinoxalin-2-yl)-benzenesulfonamide derivatives as phosphatidylinositol 3-kinase inhibitors
NZ566903A (en) * 2005-10-07 2011-09-30 Exelixis Inc Pyrido (2,3-D) pyrimidinone compounds and their use as PI3 inhibitors
CN101365676B (en) * 2005-10-07 2013-09-11 埃克塞利希斯股份有限公司 Azetidines as mek inhibitors for the treatment of proliferative diseases
AU2013201011B2 (en) * 2005-10-07 2016-04-21 Exelixis, Inc. N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
GB0601962D0 (en) 2006-01-31 2006-03-15 Ucb Sa Therapeutic agents
ATE539752T1 (en) 2006-08-16 2012-01-15 Exelixis Inc USE OF PI3K AND MEK MODULATORS IN CANCER TREATMENT
PT2074122E (en) 2006-09-15 2011-08-24 Pfizer Prod Inc Pyrido (2, 3-d) pyrimidin0ne compounds and their use as pi3 inhibitors
TR201900306T4 (en) * 2006-12-14 2019-02-21 Exelixis Inc Methods of using Mek inhibitors.
CA2675884C (en) * 2007-02-22 2016-04-26 Merck Serono S.A. Quinoxaline compounds and use thereof
WO2008124085A2 (en) * 2007-04-03 2008-10-16 Exelixis, Inc. Methods of using combinations of mek and jak-2 inhibitors
ES2430614T3 (en) * 2007-04-10 2013-11-21 Exelixis, Inc. Cancer treatment methods using PI3K alpha pyridopyrimidinone inhibitors
AU2008239655B2 (en) * 2007-04-11 2013-06-20 Exelixis, Inc. Pyrido (2, 3-d) pyrimidin-7-one compounds as inhibitors of PI3k-alpha for the treatment of cancer
CN101711249A (en) * 2007-04-11 2010-05-19 埃克塞里艾克西斯公司 Pyrido [2,3-D] the pyrimidin-7-ones compound that is used for the treatment of cancer as the inhibitor of PI3K-α
UA98141C2 (en) 2007-04-11 2012-04-25 Экселиксис, Инк. Methods of treating with quinaxoline inhibitors of pi3k-alpha
WO2009017838A2 (en) * 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
WO2009139886A2 (en) * 2008-05-14 2009-11-19 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Targeting an hiv-1 nef-host cell kinase complex
GB0815947D0 (en) 2008-09-02 2008-10-08 Univ Dundee Compounds
US8476282B2 (en) * 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
ES2463676T3 (en) 2008-11-10 2014-05-28 Kyowa Hakko Kirin Co., Ltd. Quinurenine production inhibitor
WO2010068738A1 (en) 2008-12-10 2010-06-17 Dana-Farber Cancer Institute, Inc. Mek mutations conferring resistance to mek inhibitors
CA2772790C (en) 2009-09-04 2017-06-27 Benjamin Bader Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors
EP2482819A4 (en) * 2009-09-28 2013-02-20 Glaxosmithkline Llc Combination
TWI428336B (en) * 2009-10-12 2014-03-01 Hoffmann La Roche Combination of PI3K inhibitor and MEK inhibitor
TW201139436A (en) * 2010-02-09 2011-11-16 Exelixis Inc Methods of treating cancer using pyridopyrimidinone inhibitors of PI3K and mTOR in combination with autophagy inhibitors
RU2571930C2 (en) 2010-02-25 2015-12-27 Дана-Фарбер Кэнсер Инститьют, Инк. Braf mutations ensuing resistance to braf inhibitors
CN103038364A (en) 2010-03-09 2013-04-10 达纳－法伯癌症研究所公司 Methods of diagnosing and treating cancer in patients having or developing resistance to a first cancer therapy
US9376709B2 (en) 2010-07-26 2016-06-28 Biomatrica, Inc. Compositions for stabilizing DNA and RNA in blood and other biological samples during shipping and storage at ambient temperatures
CA2806734A1 (en) 2010-07-26 2012-02-09 Biomatrica, Inc. Compositions for stabilizing dna, rna and proteins in saliva and other biological samples during shipping and storage at ambient temperatures
CA2812089C (en) 2010-09-14 2020-02-18 Exelixis Inc. Inhibitors of pi3k-delta and methods of their use and manufacture
DE102010048800A1 (en) 2010-10-20 2012-05-10 Merck Patent Gmbh quinoxaline
US20130211076A1 (en) * 2010-10-20 2013-08-15 Merck Serono S.A. Geneva Method for preparing substituted N-(3-amino-quinoxalin-2-yl)-sulfonamides and their intermediates N-(3-chloro-quinoxalin-2-yl)-sulfonamides
WO2012065057A2 (en) * 2010-11-12 2012-05-18 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors and methods of their use
BR112013012485A2 (en) * 2010-11-19 2016-09-06 Glaxosmithkline Ip No 2 Ltd braf inhibitor treatment method
CN102718750B (en) * 2011-03-31 2015-03-11 中国人民解放军军事医学科学院毒物药物研究所 Aminopyridine derivatives containing acridine ring and application thereof
MX351133B (en) 2011-09-22 2017-10-03 Exelixis Inc Method for treating osteoporosis.
PH12014500973A1 (en) 2011-11-01 2014-06-16 Exelixis Inc Phosphatidylinositol 3-kinase inhibitors for the treatment of lymphoproliferative malignancies
WO2013067306A1 (en) * 2011-11-02 2013-05-10 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors for the treatment of childhood cancers
CN103204825B (en) 2012-01-17 2015-03-04 上海科州药物研发有限公司 Benzothiazole compounds as protein kinase inhibitors, and preparation method and application thereof
WO2013135612A1 (en) 2012-03-14 2013-09-19 Bayer Intellectual Property Gmbh Substituted imidazopyridazines
US20150141470A1 (en) 2012-05-08 2015-05-21 The Broad Institute, Inc. Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy
US9611267B2 (en) 2012-06-13 2017-04-04 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
JP6300042B2 (en) 2012-10-12 2018-03-28 エグゼリクシス， インコーポレイテッド Method for producing a compound for use in the treatment of cancer
AU2013337702A1 (en) 2012-11-02 2015-05-21 Merck Patent Gmbh Method of reducing adverse effects in a cancer patient undergoing treatment with a MEK inhibitor
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
US9725703B2 (en) 2012-12-20 2017-08-08 Biomatrica, Inc. Formulations and methods for stabilizing PCR reagents
BR112015023203A8 (en) 2013-03-15 2018-01-23 Constellation Pharmaceuticals Inc methods for treating cancer, method for increasing the efficiency of cancer treatment, method for delaying and / or preventing cancer development, method for treating an individual with cancer, method for increasing sensitivity for a cancer therapy agent, method for extending a sensitivity period and method for extending the duration of response to cancer therapy.
MA38654B1 (en) 2013-06-11 2018-11-30 Bayer Pharma AG Derivatives of the prodrug type of substituted triazolopyridines
CN105491883B (en) 2013-06-13 2018-11-02 生物马特里卡公司 Cell stabilization
RU2715236C2 (en) 2014-03-26 2020-02-26 Астекс Терапьютикс Лтд Combinations
JP6661554B2 (en) 2014-06-10 2020-03-11 バイオマトリカ，インク． Platelet stabilization at ambient temperature
WO2015196072A2 (en) 2014-06-19 2015-12-23 Whitehead Institute For Biomedical Research Uses of kinase inhibitors for inducing and maintaining pluripotency
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
JOP20200201A1 (en) 2015-02-10 2017-06-16 Astex Therapeutics Ltd Pharmaceutical compositions comprising n-(3,5-dimethoxyphenyl)-n'-(1-methylethyl)-n-[3-(1-methyl-1h-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine
MA41551A (en) 2015-02-20 2017-12-26 Incyte Corp BICYCLIC HETEROCYCLES USED AS FGFR4 INHIBITORS
ES2751669T3 (en) 2015-02-20 2020-04-01 Incyte Corp Bicyclic heterocycles as FGFR inhibitors
AR105483A1 (en) 2015-06-30 2017-10-11 Exelixis Inc CRYSTAL FUMARATE SALT OF (S) - [3,4-DIFLUORO-2- (2-FLUORO-4-IODOPHENYLAMINE) PHENYL] [3-HIDROXI-3- (PIPERIDIN-2-IL) AZETIDIN-1-IL] - METANONE
WO2017100212A1 (en) 2015-12-08 2017-06-15 Biomatrica, Inc. Reduction of erythrocyte sedimentation rate
EP3464236A4 (en) 2016-05-26 2020-01-08 The Regents of the University of California COMPOUNDS AND METHODS FOR HEMATOPOIETIC REGENERATION
WO2018183936A1 (en) * 2017-03-31 2018-10-04 The Broad Institute, Inc. Compounds and methods useful for treating or preventing cancers
JP2020520949A (en) * 2017-05-22 2020-07-16 ユニバーシティ オブ ヴァージニア パテント ファウンデーションＵｎｉｖｅｒｓｉｔｙ Ｏｆ Ｖｅｒｇｉｎｉａ Ｐａｔｅｎｔ Ｆｏｕｎｄａｔｉｏｎ Compositions and methods of preparing and using mitochondrial uncouplers
AR111960A1 (en) 2017-05-26 2019-09-04 Incyte Corp CRYSTALLINE FORMS OF A FGFR INHIBITOR AND PROCESSES FOR ITS PREPARATION
US20210188763A1 (en) * 2017-11-29 2021-06-24 The Regents Of The University Of California Compounds and methods for hematopoietic regeneration
SG11202010636VA (en) 2018-05-04 2020-11-27 Incyte Corp Solid forms of an fgfr inhibitor and processes for preparing the same
KR20210018264A (en) 2018-05-04 2021-02-17 인사이트 코포레이션 Salts of FGFR inhibitors
JP7304896B2 (en) * 2018-05-21 2023-07-07 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ Heterofused pyridone compounds and their use as IDH inhibitors
CN113660931B (en) * 2018-11-20 2024-10-11 恩福莱克逊治疗有限公司 Arylaniline and heteroarylaniline compounds for the treatment of skin cancer
EP3911313A4 (en) * 2018-11-20 2022-10-12 NFlection Therapeutics, Inc. Thienyl-aniline compounds for treatment of dermal disorders
MA55141A (en) 2018-11-20 2021-09-29 Nflection Therapeutics Inc CYANOARYL-ANILINE COMPOUNDS FOR THE TREATMENT OF SKIN CONDITIONS
WO2020106307A1 (en) * 2018-11-20 2020-05-28 Nflection Therapeutics, Inc. Aryl-aniline and heteroaryl-aniline compounds for treatment of birthmarks
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
PE20221085A1 (en) 2019-10-14 2022-07-05 Incyte Corp BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
JP2022554364A (en) 2019-11-08 2022-12-28 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ Gem-disubstituted heterocyclic compounds and their use as IDH inhibitors
BR112022010664A2 (en) 2019-12-04 2022-08-16 Incyte Corp DERIVATIVES OF A FGFR INHIBITOR
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
ES2836551A1 (en) * 2020-08-11 2021-06-25 Molik Candelo Holmes Andreaquivi drug C34H34N6O6S (Machine-translation by Google Translate, not legally binding)
TW202304459A (en) 2021-04-12 2023-02-01 美商英塞特公司 Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
JP2024522189A (en) 2021-06-09 2024-06-11 インサイト・コーポレイション Tricyclic Heterocycles as FGFR Inhibitors
JP2024526791A (en) * 2021-07-16 2024-07-19 セレーター ファーマシューティカルズ インコーポレイテッド Method for preparing liposomal formulations

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040009993A1 (en) * 2001-12-11 2004-01-15 Pharmacia Italia S.P.A. Pyridopyrimidinones derivatives as telomerase inhibitors
WO2006044453A1 (en) * 2004-10-13 2006-04-27 Wyeth Analogs of 17-hydroxywortmannin as pi3k inhibitors
WO2006045514A1 (en) * 2004-10-20 2006-05-04 Applied Research Systems Ars Holding N.V. 3-arylamino pyridine derivatives
WO2007044698A1 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα
WO2007044515A1 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. Azetidines as mek inhibitors for the treatment of proliferative diseases
WO2007044729A2 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998033798A2 (en) 1997-02-05 1998-08-06 Warner Lambert Company Pyrido[2,3-d]pyrimidines and 4-amino-pyrimidines as inhibitors of cell proliferation
BR9810385A (en) * 1997-07-01 2000-09-05 Warner Lambert Co Derivatives of benzoic acid 2- (4-bromine or 4-iodine phenylamino) and their use as mek inhibitors
WO2005105801A1 (en) 2004-05-04 2005-11-10 Warner-Lambert Company Llc Pyrrolyl substituted pyrido[2,3-d]pyrimidin-7-ones and derivatives thereof as therapeutic agents
CN101296909B (en) 2005-08-26 2011-10-12 默克雪兰诺有限公司 Pyrazine derivatives and use as pI3K inhibitors
NZ566903A (en) 2005-10-07 2011-09-30 Exelixis Inc Pyrido (2,3-D) pyrimidinone compounds and their use as PI3 inhibitors
ATE539752T1 (en) 2006-08-16 2012-01-15 Exelixis Inc USE OF PI3K AND MEK MODULATORS IN CANCER TREATMENT
TR201900306T4 (en) * 2006-12-14 2019-02-21 Exelixis Inc Methods of using Mek inhibitors.
ES2430614T3 (en) 2007-04-10 2013-11-21 Exelixis, Inc. Cancer treatment methods using PI3K alpha pyridopyrimidinone inhibitors
CN101711249A (en) 2007-04-11 2010-05-19 埃克塞里艾克西斯公司 Pyrido [2,3-D] the pyrimidin-7-ones compound that is used for the treatment of cancer as the inhibitor of PI3K-α
UA98141C2 (en) 2007-04-11 2012-04-25 Экселиксис, Инк. Methods of treating with quinaxoline inhibitors of pi3k-alpha
AU2008239655B2 (en) 2007-04-11 2013-06-20 Exelixis, Inc. Pyrido (2, 3-d) pyrimidin-7-one compounds as inhibitors of PI3k-alpha for the treatment of cancer
JP2012504628A (en) 2008-09-30 2012-02-23 エグゼリクシス， インコーポレイテッド Pyridopyrimidinone inhibitors of PI3Kα and mTOR
TW201139436A (en) 2010-02-09 2011-11-16 Exelixis Inc Methods of treating cancer using pyridopyrimidinone inhibitors of PI3K and mTOR in combination with autophagy inhibitors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040009993A1 (en) * 2001-12-11 2004-01-15 Pharmacia Italia S.P.A. Pyridopyrimidinones derivatives as telomerase inhibitors
WO2006044453A1 (en) * 2004-10-13 2006-04-27 Wyeth Analogs of 17-hydroxywortmannin as pi3k inhibitors
WO2006045514A1 (en) * 2004-10-20 2006-05-04 Applied Research Systems Ars Holding N.V. 3-arylamino pyridine derivatives
WO2007044698A1 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα
WO2007044515A1 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. Azetidines as mek inhibitors for the treatment of proliferative diseases
WO2007044729A2 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SHELTON J G ET AL: "ssffects of the RAF/MEK/ERK and PI3K/AKT signal transduction pathways o", ONCOGENE, BASINGSTOKE, HANTS, GB, vol. 22, no. 16, 24 April 2003 (2003-04-24), pages 2478 - 2492, XP002402152, ISSN: 0950-9232 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9533954B2 (en) 2010-12-22 2017-01-03 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
US9533984B2 (en) 2013-04-19 2017-01-03 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors

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